CN114786674A - Ahr抑制剂和pd1抑制剂抗体的组合及其在癌症治疗中的用途 - Google Patents

Ahr抑制剂和pd1抑制剂抗体的组合及其在癌症治疗中的用途 Download PDF

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CN114786674A
CN114786674A CN202080084993.9A CN202080084993A CN114786674A CN 114786674 A CN114786674 A CN 114786674A CN 202080084993 A CN202080084993 A CN 202080084993A CN 114786674 A CN114786674 A CN 114786674A
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oxo
carboxamide
dihydropyridazine
pyridin
chlorophenyl
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Chinese (zh)
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I·古彻
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Bayer AG
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Bayer AG
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39541Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against normal tissues, cells
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2827Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/21Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/70Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/70Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/73Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/70Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76Antagonist effect on antigen, e.g. neutralization or inhibition of binding

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Immunology (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
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  • Microbiology (AREA)
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  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202080084993.9A 2019-12-16 2020-12-14 Ahr抑制剂和pd1抑制剂抗体的组合及其在癌症治疗中的用途 Pending CN114786674A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962948430P 2019-12-16 2019-12-16
EP19216672.6 2019-12-16
EP19216672 2019-12-16
US62/948,430 2019-12-16
PCT/EP2020/085938 WO2021122434A1 (en) 2019-12-16 2020-12-14 Combination of an ahr-inhibitor and an pd1-inhibitor antibody and its use in the treatment of cancer

Publications (1)

Publication Number Publication Date
CN114786674A true CN114786674A (zh) 2022-07-22

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CN202080084993.9A Pending CN114786674A (zh) 2019-12-16 2020-12-14 Ahr抑制剂和pd1抑制剂抗体的组合及其在癌症治疗中的用途

Country Status (11)

Country Link
US (1) US20230084899A1 (pt)
EP (1) EP4076462A1 (pt)
JP (1) JP2023505907A (pt)
KR (1) KR20220128622A (pt)
CN (1) CN114786674A (pt)
AU (1) AU2020403801A1 (pt)
BR (1) BR112022007837A2 (pt)
CA (1) CA3164474A1 (pt)
IL (1) IL293861A (pt)
MX (1) MX2022007438A (pt)
WO (1) WO2021122434A1 (pt)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114835687A (zh) * 2021-04-02 2022-08-02 重庆华森制药股份有限公司 AhR抑制剂

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105461687A (zh) * 2014-08-26 2016-04-06 沈阳中海生物技术开发有限公司 含二氢哒嗪酮的喹啉类化合物及其用途
WO2018146010A1 (en) * 2017-02-09 2018-08-16 Bayer Aktiengesellschaft 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer
WO2019101643A1 (en) * 2017-11-21 2019-05-31 Bayer Aktiengesellschaft 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyridazine-4-carboxamides
WO2019101642A1 (en) * 2017-11-21 2019-05-31 Bayer Aktiengesellschaft Sulphur substituted 3-oxo-2,3-dihydropyridazine-4-carboxamides
CN109863140A (zh) * 2016-05-25 2019-06-07 拜耳医药股份有限公司 3-氧代-2,6-二苯基-2,3-二氢哒嗪-4-甲酰胺

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5011472A (en) 1988-09-06 1991-04-30 Brown University Research Foundation Implantable delivery system for biological factors
SI2161336T1 (sl) 2005-05-09 2013-11-29 Ono Pharmaceutical Co., Ltd. Humana monoklonska protitelesa za programirano smrt 1 (PD-1) in postopki za zdravljenje raka ob uporabi anti-PD-1 protiteles samih ali v kombinaciji z drugimi imunoterapevtiki
EP2535354B1 (en) 2007-06-18 2017-01-11 Merck Sharp & Dohme B.V. Antibodies to human programmed death receptor pd-1

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105461687A (zh) * 2014-08-26 2016-04-06 沈阳中海生物技术开发有限公司 含二氢哒嗪酮的喹啉类化合物及其用途
CN109863140A (zh) * 2016-05-25 2019-06-07 拜耳医药股份有限公司 3-氧代-2,6-二苯基-2,3-二氢哒嗪-4-甲酰胺
WO2018146010A1 (en) * 2017-02-09 2018-08-16 Bayer Aktiengesellschaft 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer
WO2019101643A1 (en) * 2017-11-21 2019-05-31 Bayer Aktiengesellschaft 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyridazine-4-carboxamides
WO2019101642A1 (en) * 2017-11-21 2019-05-31 Bayer Aktiengesellschaft Sulphur substituted 3-oxo-2,3-dihydropyridazine-4-carboxamides

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114835687A (zh) * 2021-04-02 2022-08-02 重庆华森制药股份有限公司 AhR抑制剂
CN114835687B (zh) * 2021-04-02 2023-09-05 北京华森英诺生物科技有限公司 AhR抑制剂

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Publication number Publication date
BR112022007837A2 (pt) 2022-07-05
US20230084899A1 (en) 2023-03-16
WO2021122434A1 (en) 2021-06-24
JP2023505907A (ja) 2023-02-13
AU2020403801A1 (en) 2022-06-02
MX2022007438A (es) 2022-07-19
KR20220128622A (ko) 2022-09-21
CA3164474A1 (en) 2021-06-24
EP4076462A1 (en) 2022-10-26
IL293861A (en) 2022-08-01

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